Fluperamide is a synthetic

opioid Opioids are a class of Drug, drugs that derive from, or mimic, natural substances found in the Papaver somniferum, opium poppy plant. Opioids work on opioid receptors in the brain and other organs to produce a variety of morphine-like effects, ...

structurally related to

loperamide Loperamide, sold under the brand name Imodium, among others,Drugs.co Page accessed 4 September 2015 is a medication of the opioid receptor agonist class used to decrease the frequency of diarrhea. It is often used for this purpose in irritable ...

, developed as a potent

antidiarrheal Antidiarrheals are a class of medication used primarily to manage and reduce the frequency of diarrhea. This class of medication predominantly works by slowing digestion, reducing fluid loss, or improving absorption. There are four main classes: op ...

agent. Like loperamide, it acts primarily as a peripherally selective

μ-opioid receptor The μ-opioid receptors (MOR) are a class of opioid receptors with a high affinity for enkephalins and beta-endorphin, but a low affinity for dynorphins. They are also referred to as μ(''mu'')-opioid peptide (MOP) receptors. The prototypical ...

agonist, effectively reducing

gastrointestinal motility Gastrointestinal physiology is the branch of Human body, human physiology that addresses the physical function of the Human gastrointestinal tract, gastrointestinal (GI) tract. The function of the GI tract is to process ingested food by mechanical ...

and fluid secretion without significant

central nervous system The central nervous system (CNS) is the part of the nervous system consisting primarily of the brain, spinal cord and retina. The CNS is so named because the brain integrates the received information and coordinates and influences the activity o ...

effects due to limited blood-brain barrier penetration. Fluperamide’s pharmacological profile was designed to maximize antidiarrheal efficacy while minimizing the risk of opioid-related side effects and abuse potential, a strategy that has contributed to the development of related compounds in the

phenylpiperidine Phenylpiperidines are chemical compounds with a phenyl moiety (chemistry), moiety directly attached to piperidine. Of particular interest are a variety of chemical derivative, derivatives of 4-phenylpiperidine, which have pharmacology, pharmacolo ...

class. Although fluperamide demonstrated strong antidiarrheal activity in preclinical and early clinical studies, it was ultimately not commercialized, with loperamide becoming the preferred agent in this therapeutic category due to its favorable safety and efficacy.

References

{{Opioid receptor modulators 4-Phenylpiperidines Antidiarrhoeals Belgian inventions Butyramides Janssen Pharmaceutica Mu-opioid receptor agonists Synthetic opioids Tertiary alcohols Trifluoromethyl compounds Dimethylamino compounds 4-Chlorophenyl compounds

See also

References